4-morpholinecarboximidine-N-1-adamantyl-N-cyclohexyl | 122252-09-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 英文名称: 4-morpholinecarboximidine-N-1-adamantyl-N-cyclohexyl
• 英文别名: N-(1-adamantyl)-N'-cyclohexyl-4-morpholinecarboxamidine；PNU-37883A；N-adamantan-1-yl-morpholine-4-carboximidic acid cyclohexylamide；N'-(ADamantan-1-yl)-N-cyclohexylmorpholine-4-carboximidamide；N-(1-adamantyl)-N'-cyclohexylmorpholine-4-carboximidamide
• CAS: 122252-09-9
• 化学式: C₂₁H₃₅N₃O
• 分子量: 345.528
• InChiKey: GKCGWXNLOYTUNC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  25
• 可旋转键数：
  4
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.95
• 拓扑面积：
  36.9
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  N-(1-adamantyl)-N'-cyclohexylthiourea 在 COCl₂ 作用下， 以 四氢呋喃 、 氯仿 、 乙腈 为溶剂， 反应 23.5h， 生成 4-morpholinecarboximidine-N-1-adamantyl-N-cyclohexyl
  参考文献：
  名称：

  N，N'-二环己基-4-吗啉羧box的烷基和芳基胍类似物的合成及其利尿活性。

  摘要：

  随机筛选确定N，N'-二环己基-4-吗啉羧box（U-18177，1）为大鼠口服有效的非利尿剂利尿剂。在狗中口服1和其1-金刚烷基类似物（U-37883A，4）的利尿特性时，它们的功效不如标准利尿剂，但在>或= 100 mumol / kg时显示了速尿类似的利尿作用。但是，急性1在61和90 mumol / kg iv静脉注射可导致犬致命的心脏毒性。1的许多类似物在质上表现出相似的利尿特性，但没有一个足以保证发育。化合物1还逆转了米诺地尔在犬中的血管舒张作用，这导致了血管相互作用的研究表明，类似物4可能会阻断ATP敏感的K通道。这种钾通道阻滞机制可能有助于该系列的利尿活性。

  DOI：

  10.1021/jm00048a005

文献信息

• Fluoro-substituted adamantane derivatives
  申请人：PFIZER INC.

  公开号：EP0870757B1

  公开（公告）日：2002-06-12
• Compositions and methods for the treatment of neurodegenerative diseases
  申请人：Staunton Jane

  公开号：US20060270742A1

  公开（公告）日：2006-11-30

  The invention features compositions and methods for the treatment of neurodegenerative diseases.
• Intranasal administration of modulators of hypothalamic ATP-sensitive potassium channels
  申请人：Herlands Louis

  公开号：US20070026079A1

  公开（公告）日：2007-02-01

  Provided are methods of increasing K ATP channel activity in the hypothalamus of a mammal, methods of reducing glucose production in a mammal, methods of reducing peripheral glucose levels in a mammal, methods of reducing triglyceride levels in a mammal, methods of reducing very low density lipoprotein (VLDL) levels in a mammal, methods of methods of reducing gluconeogenesis in the liver of a mammal, methods of treating metabolic disorders such as diabetes, hyperglycemia, insulin resistance, glucose intolerance, metabolic syndrome and/or obesity, and methods of increasing glucose production and peripheral glucose levels in a mammal. Also provided are methods of treating heart failure, ischemia, coronary heart disease, familial lipoprotein lipase deficiency, hypopituitarism, hyperlipidemia, hypertriglyceridemia, hyperVLDLemia, atherosclerosis, hypercholesterolemia, hypertension, polycystic ovary syndrome, gonadotropin deficiency and/or amenorrhea.
• Modulation of Hypothalamic Atp-Sensitive Potassium Channels
  申请人：Rossetti Luciano

  公开号：US20090012067A1

  公开（公告）日：2009-01-08

  Provided are methods of increasing K ATP activity in the hypothalamus of a mammal, methods of reducing glucose production and peripheral blood glucose levels in a mammal, methods of inhibiting gluconeogenesis in the liver of a mammal, and methods of increasing glucose production and peripheral blood glucose levels in a mammal.
• Compositions, Methods, and Kits for Treating Influenza Viral Infections
  申请人：Altmeyer Ralf

  公开号：US20110028510A1

  公开（公告）日：2011-02-03

  The present invention provides compositions, methods, and kits for treating or preventing a viral infection (e.g., an infection caused by an influenza virus).